Design and synthesis of new Nilutamide-1,2,3-triazole derivatives as in vitro Anticancer agents
The synthesis of novel 1,2,3-triazoles of Nilutamide (4a–4n) via Cu(I)-promoted 1,3-dipolar cycloaddition reaction between several terminal alkynes and 1-(3-azidopropyl)-5,5-dimethyl-3-(4-nitro-3-(trifluoromethyl)phenyl)imidazolidine-2,4-dione have been reported herein. In vitro anticancer activity studies of these synthesized compounds over two human prostate cell lines PC3 and DU-145 revealed that the compounds 4c, 4f and 4n exhibit slightly greater activity against two cell lines than the standard etoposide. Predominantly, the compound 4f displayed excellent activity over PC3 and DU-145 having IC50 values of 1.84and 1.34 μM respectively. The three most potent compounds 4c, 4f and 4n were also investigated for their inhibitory potential against tyrosine kinase EGFR and found that compound 4f showed superior activity than the standard erlotinib, while remaining two compounds 4c and 4n showed comparable activity with the standard.
Design and synthesis of new Nilutamide-1,2,3-triazole derivatives as in vitro Anticancer agents – https://pubs.thesciencein.org/journal/index.php/cbl/article/view/405
Chemical Biology Letters
Design, synthesis and molecular docking studies of new Quinoxaline-linked-1,2,4-triazole-Sulfonamide hybrids as Anti-proliferative agents
A new series of quinoxaline linked 1,2,4-triazole sulfonamide derivatives were designed and efficiently synthesized. All compounds were characterized by their IR, 1HNMR, 13CNMR, and Mass spectral data, and elemental analysis. The final compounds (5a-m) were screened for in vitro anti-proliferative activity against cancer cell lines HeLa (lung), A549 (carcinoma), MCF-7 (breast) and HCT116 (colon).The results revealed that the compounds 5k, 5l and 5d have shown promising activity as compared to etoposide. Predominantly, the compound 5k displayed greater activity on HeLa, A549, MCF-7and HCT116 with IC50 values of 1.97±0.09, 1.84±0.07, 3.10±0.04and 4.10±0.07 than the standard drug etoposide. Moreover, molecular docking studies of 5k, 5l and 5d on EGFR receptor suggested that the most potent compound 5k strongly binds to protein EGFR (pdbid: 4HJO). Furthermore, the compounds 5k and 5l displayed promising inhibitory activity over tyrosine kinase EGFR when compared with the standard erlotinib.
Design, synthesis and molecular docking studies of new Quinoxaline-linked-1,2,4-triazole-Sulfonamide hybrids as Anti-proliferative agents – https://pubs.thesciencein.org/journal/index.php/cbl/article/view/396
Chemical Biology Letters
The evolution of lipid nanoparticles (LNPs) has been remarkably interesting and in beneficent directions for food and health industries working towards human well being. Since the discovery of the first-generation lipid based self-assembled nanostructures, i.e., liposomes in the 1960s, it has witnessed significant advances in their development and distinctive potential in different application domains. Based on the composition and structure, these lipid based structures have varied from liposome to lipid nanoparticles such as nanostructured lipid carriers (NLCs) and solid lipid nanoparticles (SLN) to overcome certain limitation pertaining to their use in different fields. The outstanding application of LNPs as therapeutic delivery systems has made them key players to treat different human disorders including the fatal cancers. Their life-saving global contribution has recently been witnessed in the form of mRNA vaccines against deadly COVID-19. They have also significantly served purpose in other domains such as biomedical imaging, cosmetics, nutrition, and agriculture. Their prominent role is in the area of anticancer therapy as delivery vectors for nucleic acids and drugs. Some issues with respect to the cellular delivery of drugs and genes, such as circulation time and stability have been somewhat resolved, but the unmet goal of site-specific substantial delivery remains the main focus in LNPs development research. Despite the promise shown by LNPs in animal studies and the fact that technological advances in LNPs research have made the approval possible of a few formulations, therapeutic outcomes in human are not satisfactory. The LNPs technology has managed to survive due to possible tailoring of their properties by virtue of the possibility of altering the composition and modifying the surface. Therefore, enormous scientific endeavours are on the rise to transform lipid structures, composition along with tinkering with surface of LNPs. The alternative methods to guide LNPs coupled with advances in small molecule nucleic acid therapeutics and drug development technology to make the entry possible to specific cells may be effective in cancer therapy. The development is very promising; however enduring efforts are required till the goal is reached.
Published in : Chemical Biology Letters